Lumateperone, our lead product candidate, is a first-in-class molecule that provides selective and simultaneous modulation of serotonin, dopamine, and glutamate—three neurotransmitter pathways implicated in severe mental illness. Unlike existing schizophrenia treatments, lumateperone is a dopamine receptor phosphoprotein modulation, or DPPM, acting as a pre-synaptic partial agonist and post-synaptic antagonist at D2 receptors. We believe this mechanism, along with potent interactions at 5-HT2A receptors, serotonin transporters, and D1 receptors with indirect glutamatergic modulation, contributes to the efficacy of ITI-007 across a broad array of symptoms, with improved psychosocial function and favorable tolerability. This compound has the potential to benefit patients suffering from a range of neuropsychiatric and neurodegenerative diseases.
Our clinical development program for the treatment of schizophrenia with lumateperone includes three large randomized, double-blind, placebo-controlled trials—studies ‘005, ‘301, and ‘302. In two studies, the efficacy of ITI-007 60 mg was demonstrated, showing a statistically significant separation from placebo on the primary endpoint, the Positive and Negative Syndrome Scale or PANSS total score. Across all three studies, ITI-007 was found to be well tolerated with a safety profile similar to placebo.Across all three studies, ITI-007 was found to be well tolerated with a safety profile similar to placebo Our clinical development program in bipolar depression consists of two, 6-week, Phase 3 clinical trials and includes patients with both bipolar I and bipolar II disorder. One trial, ‘401, evaluates lumateperone as a monotherapy and the other trial, ‘402, evaluates ITI-007 as an adjunctive therapy, with either lithium or valproate. Our Phase 3 clinical development program for the treatment of agitation in patients with dementia, including Alzheimer’s disease, is ongoing. The ‘201 trial includes patients with a clinical diagnosis of probable AD and clinically significant symptoms of agitation.